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【结 构 式】 
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【分子编号】13431 【品名】1-Benzyl-4-piperidinecarbaldehyde 【CA登记号】 |
【 分 子 式 】C13H17NO 【 分 子 量 】203.28412 【元素组成】C 76.81% H 8.43% N 6.89% O 7.87% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号：(II)The condensation of 5,6-dimethoxy-1-indanone (I) with 1-benzylpiperidine-4-carboxaldehyde (II) by means of butyllithium and diisopropylamine in THF gives 1-benzyl-4-(5,6-dimethoxy-1-oxoindan-2-ylidenemethyl)piperidine (III), which is reduced with H2 over Pd/C in THF and treated with HCl in dichloromethane - ethyl acetate.
| 【1】 Sugimoto, H.; Tsuchiya, Y.; Higurashi, K.; Karibe, N.; Iimura, Y.; Sasaki, A.; Yamanashi, Y.; Ogura, H.; Araki, S.; Kosasa, T.; Kusota, A.; Kozasa, M.; Yamatsu, K. (Eisai Co., Ltd.); Cyclic amine cpd., its use and pharmaceutical compsns. comprising it. AU 8818216; EP 0296560; EP 0673927; EP 0742207; JP 1989079151; JP 1998067739; US 4895841; US 5100901 . |
| 【2】 Sugimoto, H.; Mishima, M.; Iimura, Y.; Synthesis of 1-benzyl-4-[(5,6-dimethoxy[2-14C]-1-indanon)-2-yl]methylpiperidine hydrochloride (E-2020-14C). J Label Compd Radiopharm 1989, 27, 7, 835-9. |
| 【3】 Castaner, J.; Prous, J.; E-2020. Drugs Fut 1991, 16, 1, 16. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (I) | 13430 | 5,6-Dimethoxy-1-indanone; 2,3-Dihydro-5,6-dimethoxy-1H-inden-1-one | 2107-69-9 | C11H12O3 | 详情 | 详情 |
| (II) | 13431 | 1-Benzyl-4-piperidinecarbaldehyde | C13H17NO | 详情 | 详情 | |
| (III) | 13432 | 2-[(E)-(1-Benzyl-4-piperidinyl)methylidene]-5,6-dimethoxy-1-indanone | 120014-07-5 | C24H27NO3 | 详情 | 详情 |
Extended Information